Propofol formulation with enhanced microbial inhibition

A - Human Necessities – 61 – K

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A61K 31/05 (2006.01) A61K 47/24 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2397990

A sterile, stable pharmaceutical formulations of oil-in-water emulsions of Propofol containing no preservative are provided that comprise optimal amounts of egg lecithin and soybean oil, with a suitable pH range to prevent significant growth of microorganisms for at least 24 hours after adventitious, extrinsic contamination. The lower pH in the formulation has shown the most antimicrobial activity. The reduced amount of fat in the formulation also allows chronic sedation over extended periods of time with a reduced chance of fat overload in the blood.

L'invention concerne des formulations pharmaceutiques stables et st~riles d'~mulsions de type aqueux de propofol ne contenant aucun conservateur, comprenant des doses optimales d'ovol~cithine et d'huile de soja, et dont la plage de pH est appropri~e ~ empÚcher une croissance significative de micro-organismes pendant au moins 24 heures apr­s une contamination extrins­que accidentelle. Le pH le plus faible de la formulation pr~sente la plus forte activit~ antimicrobienne. La quantit~ r~duite de graisse dans la formulation permet ~galement d'obtenir une s~dation chronique pendant des p~riodes prolong~es, avec un risque r~duit de surcharge graisseuse dans le sang.

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